The online portal to the latest developments in laboratories and laboratory equipment

Tuesday, 25 January 2011

Stabilised receptor to a GPCR target

Heptares Therapeutics Ltd, a drug discovery company creating new medicines targeting G-protein-coupled receptors (GPCRs), announced today that it has successfully generated a stabilised receptor (StaR) to a GPCR target nominated by Novartis using Heptares’ proprietary StaR technology. For the first time, this important target will be accessible to structure-based drug discovery technologies and approaches, thereby presenting opportunities to discover completely novel drug leads against the target. By achieving this drug discovery milestone, Heptares will receive its first milestone payment from the Novartis Option Fund, under the terms of the option agreement signed by the two companies in 2009.
GPCRs are one of the most important families of drug targets in the pharmaceutical industry. Due to the well-known instability of GPCRs when removed from cellular membranes, however, it has proved extremely challenging to solve GPCR structures and to deploy structure-based drug discovery tools to develop superior chemistries against GPCR targets. As a result, many high-value GPCRs are poorly served, or not served at all, by available chemistries. The Heptares’ StaR platform overcomes this historical limitation by stabilising GPCRs and enabling discovery of superior molecules guided by an understanding of GPCR structures.

“The Novartis milestone represents another important validation of the Heptares StaR technology and we are pleased with the progress we have made since launching this programme with Novartis. The successful creation of a StaR means that we have a unique opportunity to discover novel and superior small molecule leads against the nominated GPCR target and we look forward to advancing our work with Novartis,” said Malcolm Weir, CEO of Heptares Therapeutics.

“The Heptares StaR drug discovery platform continues to demonstrate its power, robustness and applicability to a wide range of very valuable, yet difficult or intractable GPCRs. We are very excited to see the programme advancing into the lead discovery phase and look forward to further progress in our collaboration with Heptares,” said Anja König for the Novartis Option Fund.

Under the terms of the agreement with the Novartis Option Fund, Heptares will apply its StaR technology to a target identified by Novartis and drive a drug discovery programme against that target. The agreement includes upfront and potential milestone payments to Heptares totalling up to $200 million plus royalties. Further financial terms were not disclosed.